| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
CAL-130 targets PI3Kdelta and PI3Kgamma with IC₅0 values of 1.3 nM and 6.1 nM, respectively. It is a potent and selective inhibitor of these two class I PI3K isoforms. In the absence of PTEN phosphatase tumor suppressor function, either PI3Kgamma or PI3Kdelta alone can support leukemogenesis, whereas inactivation of both isoforms suppresses tumor formation. The compound does not significantly inhibit PI3Kalpha or PI3Kbeta at these concentrations.
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| ln Vitro |
Preferentially, the p110γ and p110δ catalytic domains are inhibited by CAL-130. For p110δ and p110γ, the IC50 values of CAL-130 were 1.3 and 6.1 nM, respectively, whereas for p110α and p110β, they were 115 and 56 nM, respectively. Other intracellular signaling pathways that are essential for overall cellular survival and function, such as p38 MAPK and insulin receptor tyrosine kinase, are not inhibited by CAL-130 [1].
CAL-130 demonstrates potent in vitro inhibition of PI3Kdelta and PI3Kgamma with IC₅0 values of 1.3 nM and 6.1 nM, respectively. The compound inhibits constitutive PI3K/Akt activation in T-cell acute lymphoblastic leukemia cells. By blocking both PI3Kgamma and PI3Kdelta isoforms, CAL-130 effectively suppresses leukemogenesis in PTEN-deficient models. The compound exhibits antiproliferative activity against cancer cell lines. |
| ln Vivo |
Interfering with the combined activities of PI3Kγ and PI3Kδ was found to have therapeutic importance when given to Lck/Ptenfl/fl mice that had T-cell acute lymphoblastic leukemia (T-ALL). The animals considered for survival experiments are not well-groomed, their white blood cell (WBC) counts are higher than 45,000 μL-1, peripheral smears show blast activity, and most circulating cells (>75%) are Thy1.2 and Thy1-sensitive. 2 Positive staining twice. Base-67. Oral CAL-130 (10 mg/kg) was given to mice every 8 hours for 7 days, after which they were monitored until they became moribund. The median survival of treated animals was extended to 45 days by CAL-130, despite the short treatment time, as opposed to 7.5 days for the control group [1].
In vivo activity data for CAL-130 are not extensively documented. Based on its mechanism as a PI3Kgamma/delta inhibitor, the compound is expected to suppress tumor growth in models of T-ALL and other malignancies where PI3K signaling is dysregulated. The compound is primarily used as a research tool to investigate PI3Kgamma-dependent signaling pathways. Further in vivo efficacy studies in xenograft models would be needed to fully characterize its antitumor activity. |
| Enzyme Assay |
The in vitro enzyme assay for PI3K inhibition typically uses recombinant PI3K isoforms (alpha, beta, gamma, delta) incubated with phosphatidylinositol-4,5-bisphosphate (PIP2) substrate and ATP. Kinase activity is measured by quantifying the production of phosphatidylinositol-3,4,5-trisphosphate (PIP3) using immunoassays, radiolabeled ATP incorporation, or fluorescence-based methods. IC₅0 values are determined by incubating varying concentrations of CAL-130 with each PI3K isoform and calculating the concentration required for 50% inhibition.
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| Cell Assay |
For in vitro cell-based assays, T-ALL cell lines or other cancer cells are cultured in appropriate medium and treated with CAL-130 Hydrochloride at various concentrations. Cells are incubated for 48-72 hours and cell proliferation is measured using MTT, CellTiter-Glo, or direct cell counting. PI3K/Akt pathway inhibition is confirmed by Western blot analysis of phosphorylated Akt (Ser473) and other downstream signaling proteins. Apoptosis may be assessed using caspase activity assays or Annexin V staining.
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| Animal Protocol |
In vivo animal studies for CAL-130 would typically involve xenograft mouse models using T-ALL or other cancer cell lines. Tumor-bearing mice are administered CAL-130 orally or intraperitoneally at various doses. Tumor volume is measured periodically, and tumor growth inhibition is assessed relative to vehicle-treated controls. At study termination, tumors are harvested for histopathological analysis and assessment of PI3K pathway inhibition by immunohistochemistry or Western blot.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CAL-130 Hydrochloride are not extensively documented. The compound has molecular weight 462.93 and molecular formula C23H23ClN₈O. It is soluble in DMSO and typically formulated for in vitro studies. The compound should be stored dry, dark, at -20degC for up to 1 year. Stock solutions in DMSO can be stored at 0-4degC for up to 1 month. The compound is shipped at ambient temperature as a non-hazardous chemical. Further PK parameters would require dedicated studies.
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| Toxicity/Toxicokinetics |
Toxicological data for CAL-130 Hydrochloride are not well characterized in the public domain. As a research chemical, standard safety precautions should be observed. The compound is for laboratory use only and not intended for human therapeutic applications. PI3K inhibitors as a class may have potential toxicities including metabolic effects and immune modulation. Comprehensive toxicity profiling would be required for therapeutic development.
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| References | |
| Additional Infomation |
CAL-130 Hydrochloride (CAS# 1431697-78-7) is a PI3Kdelta/gamma inhibitor with IUPAC name (S)-2-(1-((2-amino-9H-purin-6-yl)amino)ethyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one hydrochloride. It is used in cancer research to study PI3K signaling in T-ALL. The compound is not approved for clinical use and is strictly for laboratory research purposes. Further studies are needed to explore its therapeutic potential.
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| Molecular Formula |
C23H23CLN8O
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|---|---|
| Molecular Weight |
462.934722185135
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| Exact Mass |
462.168
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| CAS # |
1431697-78-7
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| Related CAS # |
CAL-130 Racemate;474012-90-3;CAL-130;1431697-74-3
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| PubChem CID |
71576677
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
731
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)[C@H](C)NC4=NC(=NC5=C4NC=N5)N.Cl
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| InChi Key |
XEUIGTXAJSGCRB-UQKRIMTDSA-N
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| InChi Code |
InChI=1S/C23H22N8O.ClH/c1-12-7-4-5-10-16(12)31-21(28-15-9-6-8-13(2)17(15)22(31)32)14(3)27-20-18-19(26-11-25-18)29-23(24)30-20;/h4-11,14H,1-3H3,(H4,24,25,26,27,29,30);1H/t14-;/m0./s1
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| Chemical Name |
2-[(1S)-1-[(2-amino-7H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~108.01 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (6.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1602 mL | 10.8008 mL | 21.6015 mL | |
| 5 mM | 0.4320 mL | 2.1602 mL | 4.3203 mL | |
| 10 mM | 0.2160 mL | 1.0801 mL | 2.1602 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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